CN102596916B - 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 - Google Patents
3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 Download PDFInfo
- Publication number
- CN102596916B CN102596916B CN201080048756.3A CN201080048756A CN102596916B CN 102596916 B CN102596916 B CN 102596916B CN 201080048756 A CN201080048756 A CN 201080048756A CN 102596916 B CN102596916 B CN 102596916B
- Authority
- CN
- China
- Prior art keywords
- compound
- acid
- disease
- symptom
- ethyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09174619 | 2009-10-30 | ||
EP09174619.8 | 2009-10-30 | ||
PCT/EP2010/066435 WO2011051425A1 (en) | 2009-10-30 | 2010-10-29 | N-oxide of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea |
Publications (2)
Publication Number | Publication Date |
---|---|
CN102596916A CN102596916A (zh) | 2012-07-18 |
CN102596916B true CN102596916B (zh) | 2015-06-17 |
Family
ID=41396002
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201080048756.3A Expired - Fee Related CN102596916B (zh) | 2009-10-30 | 2010-10-29 | 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 |
Country Status (7)
Country | Link |
---|---|
US (3) | US20120220600A1 (nl) |
EP (1) | EP2493864B1 (nl) |
KR (1) | KR20120101367A (nl) |
CN (1) | CN102596916B (nl) |
ES (1) | ES2524548T3 (nl) |
IN (1) | IN2012DN03180A (nl) |
WO (1) | WO2011051425A1 (nl) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
AU2013241664B2 (en) * | 2012-03-30 | 2016-05-19 | Novartis Ag | FGFR inhibitor for use in the treatment of hypophosphatemic disorders |
CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
RS56924B9 (sr) | 2013-04-19 | 2019-09-30 | Incyte Holdings Corp | Biciklični heterocikli kao fgfr inhibitori |
SG11201602183QA (en) | 2013-10-25 | 2016-05-30 | Novartis Ag | Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
CA2956270C (en) | 2014-08-18 | 2022-08-09 | Eisai R&D Management Co., Ltd. | Salt of monocyclic pyridine derivative and crystal thereof |
JP6585167B2 (ja) | 2014-10-03 | 2019-10-02 | ノバルティス アーゲー | Fgfr4阻害剤としての縮環二環式ピリジル誘導体の使用 |
US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
MX2017010673A (es) | 2015-02-20 | 2018-03-21 | Incyte Corp | Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr). |
MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
US9802917B2 (en) | 2015-03-25 | 2017-10-31 | Novartis Ag | Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide |
KR20170129757A (ko) * | 2015-03-25 | 2017-11-27 | 노파르티스 아게 | Fgfr4 억제제로서의 포르밀화 n-헤테로시클릭 유도체 |
AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
CN111712245A (zh) | 2018-03-28 | 2020-09-25 | 卫材R&D管理有限公司 | 用于肝细胞癌的治疗剂 |
EP3788047A2 (en) | 2018-05-04 | 2021-03-10 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
MX2022004513A (es) | 2019-10-14 | 2022-07-19 | Incyte Corp | Heterociclos biciclicos como inhibidores de los receptores del factor de crecimiento de fibroblastos (fgfr). |
WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
CR20220285A (es) | 2019-12-04 | 2022-10-27 | Incyte Corp | Derivados de un inhibidor de fgfr |
US11897891B2 (en) | 2019-12-04 | 2024-02-13 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
CN113185510B (zh) * | 2021-04-12 | 2022-05-13 | 南京海纳医药科技股份有限公司 | 一种阿伐曲泊帕杂质的制备方法 |
WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101336237A (zh) * | 2005-12-21 | 2008-12-31 | 诺瓦提斯公司 | 作为fgf抑制剂的嘧啶基芳基脲衍生物 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU770600B2 (en) * | 1999-10-07 | 2004-02-26 | Amgen, Inc. | Triazine kinase inhibitors |
GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
-
2010
- 2010-10-29 KR KR1020127010832A patent/KR20120101367A/ko not_active Application Discontinuation
- 2010-10-29 CN CN201080048756.3A patent/CN102596916B/zh not_active Expired - Fee Related
- 2010-10-29 EP EP10771744.9A patent/EP2493864B1/en not_active Not-in-force
- 2010-10-29 US US13/504,258 patent/US20120220600A1/en not_active Abandoned
- 2010-10-29 ES ES10771744.9T patent/ES2524548T3/es active Active
- 2010-10-29 WO PCT/EP2010/066435 patent/WO2011051425A1/en active Application Filing
- 2010-10-29 IN IN3180DEN2012 patent/IN2012DN03180A/en unknown
-
2014
- 2014-09-05 US US14/477,949 patent/US20140378468A1/en not_active Abandoned
-
2015
- 2015-12-16 US US14/971,412 patent/US20160102062A1/en not_active Abandoned
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101336237A (zh) * | 2005-12-21 | 2008-12-31 | 诺瓦提斯公司 | 作为fgf抑制剂的嘧啶基芳基脲衍生物 |
Also Published As
Publication number | Publication date |
---|---|
EP2493864B1 (en) | 2014-10-01 |
US20160102062A1 (en) | 2016-04-14 |
KR20120101367A (ko) | 2012-09-13 |
US20120220600A1 (en) | 2012-08-30 |
ES2524548T3 (es) | 2014-12-10 |
WO2011051425A1 (en) | 2011-05-05 |
EP2493864A1 (en) | 2012-09-05 |
US20140378468A1 (en) | 2014-12-25 |
CN102596916A (zh) | 2012-07-18 |
IN2012DN03180A (nl) | 2015-09-25 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN102596916B (zh) | 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 | |
EP3584239A1 (en) | O-aminoheteroaryl alkynyl-containing compound, preparation method therefor, and use thereof | |
EP3628665B1 (en) | Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase | |
EP2604610B1 (en) | Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof | |
PL189182B1 (pl) | Pochodne chinazoliny, kompozycja farmaceutyczna zawierająca pochodną chinazoliny oraz zastosowanie pochodnej chinazoliny | |
TWI325321B (en) | Combinations comprising a vegf receptor inhibitor | |
US10590109B2 (en) | Heterocyclic compounds used as FGFR inhibitors | |
MXPA01002175A (es) | Derivados de quinazolina como medicamentos. | |
CN101679313A (zh) | 用于治疗癌症或过度增殖性疾病的axl激酶抑制剂 | |
JP2012519732A (ja) | Rhoキナーゼ阻害剤 | |
CN103003250A (zh) | 作为激酶p70s6k抑制剂的二环氮杂环甲酰胺 | |
KR20120007523A (ko) | 디아미노 헤테로환 카르복사미드 화합물 | |
CN105263934A (zh) | 作为bet抑制剂的吡唑并-吡咯烷-4-酮衍生物及其在治疗疾病中的用途 | |
CN103228649A (zh) | 喹唑啉甲酰胺氮杂环丁烷 | |
US11147801B2 (en) | Methods of use for trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitors | |
Zhu et al. | Fragment-based modification of 2, 4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants | |
EP3778586A1 (en) | Quinazoline compound serving as egfr triple mutation inhibitor and applications thereof | |
EP3615027B1 (en) | Methods of use for trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitors | |
KR20100043294A (ko) | 항암제로서 사용되는 시클로펜타[g]퀴나졸린 화합물 | |
CN110016026A (zh) | 一类具有抗肿瘤活性的嘧啶并吡啶酮类化合物、制备方法和用途 | |
JP2021506935A (ja) | ピリミジン誘導体系キナーゼ阻害剤類 | |
ZA200200333B (en) | Novel carboxylic acid derivatives with 5,6 substituted pyrimidine ring, the production and utilization thereof as endothelin receptor antagonists. | |
CZ324199A3 (cs) | Léčivo k zabránění růstu solidního tumoru u člověka a způsob jeho výroby | |
JP2003500476A (ja) | アリール置換された窒素複素環を有する新規のカルボン酸誘導体、その製造およびエンドセリン受容体アンタゴニストとしてのその使用 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150617 Termination date: 20171029 |
|
CF01 | Termination of patent right due to non-payment of annual fee |